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Assay Detail

CHEMBL4605307

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to 6x-His-tagged human EphA2 ecto-domain residues (Lys27 to Asn529 residues) expressed in HEK293 cells incubated for 60 mins by fluorescence polarization assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ephrin type-A receptor 2 (CHEMBL2068)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads.
Mudd GE, Brown A, Chen L, van Rietschoten K, Watcham S, Teufel DP, Pavan S, Lani R, Huxley P, Bennett GS.
J Med Chem (2020) 63 : 4107 -4116
PubMed 32202781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.45 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4642167 1 9.27
CHEMBL4649686 1 8.82
CHEMBL4641389 1 8.70
CHEMBL4642849 1 8.55
CHEMBL4634220 1 8.55
CHEMBL4634551 1 8.51
CHEMBL4636597 1 8.32
CHEMBL4637644 1 8.29
CHEMBL4643355 1 8.28
CHEMBL4634880 1 8.26
CHEMBL4640044 1 8.24
CHEMBL4636032 1 8.24
CHEMBL4648601 1 8.24
CHEMBL4643893 1 8.17
CHEMBL4637500 1 8.05
CHEMBL4643498 1 7.89
CHEMBL4635897 1 7.84
CHEMBL4638336 1 7.58
CHEMBL4642586 1 7.46
CHEMBL4642437 1 7.41
CHEMBL4644287 1 7.25
CHEMBL4639187 1 7.09
CHEMBL4645672 1 7.08
CHEMBL4637860 1 7.08
CHEMBL4647046 1 7.00
CHEMBL4641388 1 6.94
CHEMBL4638181 1 6.80
CHEMBL4635141 1 6.68
CHEMBL4645245 1 6.65
CHEMBL4638393 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4642167 Ki = 0.54 nM 9.27
CHEMBL4649686 Ki = 1.5 nM 8.82
CHEMBL4641389 Ki = 2.0 nM 8.70
CHEMBL4642849 Ki = 2.83 nM 8.55
CHEMBL4634220 Ki = 2.8 nM 8.55
CHEMBL4634551 Ki = 3.1 nM 8.51
CHEMBL4636597 Ki = 4.8 nM 8.32
CHEMBL4637644 Ki = 5.07 nM 8.29
CHEMBL4643355 Ki = 5.2 nM 8.28
CHEMBL4634880 Ki = 5.5 nM 8.26
CHEMBL4640044 Ki = 5.78 nM 8.24
CHEMBL4648601 Ki = 5.8 nM 8.24
CHEMBL4636032 Ki = 5.74 nM 8.24
CHEMBL4643893 Ki = 6.8 nM 8.17
CHEMBL4637500 Ki = 9.0 nM 8.05
CHEMBL4643498 Ki = 12.9 nM 7.89
CHEMBL4635897 Ki = 14.5 nM 7.84
CHEMBL4638336 Ki = 26.5 nM 7.58
CHEMBL4642586 Ki = 34.5 nM 7.46
CHEMBL4642437 Ki = 39.1 nM 7.41
CHEMBL4644287 Ki = 56.1 nM 7.25
CHEMBL4639187 Ki = 81.7 nM 7.09
CHEMBL4645672 Ki = 82.5 nM 7.08
CHEMBL4637860 Ki = 83.4 nM 7.08
CHEMBL4647046 Ki = 101.0 nM 7.00
CHEMBL4641388 Ki = 115.0 nM 6.94
CHEMBL4638181 Ki = 160.0 nM 6.80
CHEMBL4635141 Ki = 210.0 nM 6.68
CHEMBL4645245 Ki = 223.0 nM 6.65
CHEMBL4638393 Ki = 263.0 nM 6.58
CHEMBL4648501 Ki = 268.0 nM 6.57
CHEMBL4632996 Ki = 539.0 nM 6.27
CHEMBL4649266 Ki = 815.0 nM 6.09
CHEMBL4639176 Ki = 931.0 nM 6.03
CHEMBL4633239 Ki = 2439.0 nM 5.61
CHEMBL4637447 Ki = 2618.0 nM 5.58
CHEMBL4634115 Ki = 3102.0 nM 5.51